TNO155 is an allosteric inhibitor of the SHP2 phosphatase, which has been a hot target in oncology recently due to its promotion of mutant KRAS activity as well as its potential role in cancer immune evasion. Phosphatases have been notoriously difficult to drug however, with reported phosphatase active site inhibitors typically having low [...]
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Sep. 18, 2021
TNO155: A First-in-Class Allosteric SHP2 Phosphatase Inhibitor
TNO155
first-in-class allosteric SHP2 phosphatase inh. oral agent in multiple trials for cancer from 1.5M cmpd biochemical HTS + SBDD J. Med. Chem., Sep. 24, 2020 Novartis, Cambridge, MA